Synthesis and biological evaluation of 1,3,4-oxadiazole Linked Thiazole-Isoxazole-Pyridines as anticancer agents

Krishna Reddy Gankidi, S. Shivakumara,K. Ramakrishna Reddy,Laxminarayana Eppakayala

RESULTS IN CHEMISTRY(2024)

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Abstract
A new library of 1,3,4-oxadiazole moiety incorporated thiazol-isoxazol-pyridine derivatives (9a-j) have been synthesized and assessed for preliminary anticancer applications against four human cancer cell lines such as PC3 (prostate cancer), A549 (lung cancer), MCF-7 (breast cancer) and SiHa (cervix cancer) by using MTT method. The obtained results were compared with chemotherapeutic agent as etoposide. The results indicated that most of the derivatives exhibited more potent activities than with standard reference. The IC50 values ranges of the compounds from 0.01 +/- 0.009 mu M to 10.8 +/- 6.23 mu M, as well as standard showed IC50 values from 2.11 +/- 0.024 mu M to 3.11 +/- 0.11 mu M. Among all, compounds 9c, 9d, 9e, 9f and 9 g demonstrated more potency of activities than etoposide. In which one compound 9c showed good anticancer activity. Docking studies also presented for the compounds synthesized.
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Key words
Crizotinib,Pyridine,Zibotentan,4-oxadiazole and anticancer
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